Cat. No. |
Product Name |
Information |
PC-35861 |
THIQ 40
ERα inhibitor
|
THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation). |
PC-35370 |
LY500307
ERβ agonist
|
LY500307 (LY-500307, Erteberel, SERBA-1) is a potent, selective Estrogen Receptor β (ERβ) agonist with Ki/EC50 of 0.19/0.66 nM, 12-fold higher affinity than ERα and exhibits 32-fold more functional potency. |
PC-35365 |
H3B-5942
ERα inhibitor
|
H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA) with Ki 1 nM and 0.41 nM for wild-type and mutant ERα Y537S respectively, covalently targeting Cys530. |
PC-35243 |
OP-1074
SERD
|
OP-1074 (OP1074) is a potent, selective ER degrader (SERD), shows specific antiestrogenic activity for both ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively. |
PC-63294 |
GDC-0927
SERD
|
GDC-0927 (SRN-927, RG6047) is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with IC50 of 0.1 nM (ER-α degradation) and Emax=97%. |
PC-63293 |
LSZ102
|
LSZ102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with ERα transcription IC50 of 6 nM and ERα degradation IC50 of 0.2 nM. |
PC-43264 |
GDC-0810
SERD
|
GDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation), binds to ERα and ERβ with with Ki of 3.8 and 3.7 nM, respectively. |
PC-43234 |
BHPI
ERα inhibitor
|
BHPI is a potent, noncompetitive small molecule ERα inhibitor (biomodulator) that selectively blocks proliferation of drug-resistant ERα-positive breast and ovarian cancer cells. |
PC-43041 |
Diarylpropionitrile
ERβ agonist
|
Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β(ERβ) selective ligand, demonstrates the neuroprotective effects against 10 0M Aβ1-42-induced oxidative stress and inflammation in primary rat cortical cell culture. |
PC-42344 |
WAY-200070
ERβ agonist
|
WAY-200070 is a potent, highly selective ERβ agonist with IC50 of 3 nM, displays 68-fold selectivity over ERα (IC50=260 nM). |
PC-70134 |
4-Hydroxytamoxifen
SERM
|
4-Hydroxytamoxifen (Afimoxifene) is a selective estrogen receptor modulator (SERM) and the major active metabolite of tamoxifen. |
PC-70133 |
Droloxifene
SERM
|
Droloxifene (3-Hydroxytamoxifen; FK-435) is a nonsteroidal selective estrogen receptor modulator (SERM) that shows 10- to 60-fold increased affinity for the estrogen receptor compared with Tamoxifen. |